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Drug Delivery to the Central Nervous System: From Design, Synthesis, and Evaluation

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Molecular Neurobiology".

Deadline for manuscript submissions: closed (30 April 2024) | Viewed by 2026

Special Issue Editor

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Guest Editor
HUN-REN-SZTE Neuroscience Research Group, Hungarian Research Network, University of Szeged (HUN-REN-SZTE), Szeged, Hungary
Interests: neurohormones; neuropeptides; tryptophan; kynurenine; psychiatry; neurology; depression; anxiety; dementia; pain; Alzheimer’s disease; cognition; antidepressant; translational research
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Special Issue Information

Dear Colleagues,

The central nervous system (CNS) is the most mysterious and fascinating organ system in the human body responsible for regulating a myriad of vital functions and enabling higher cognitive processes. However, the CNS is also highly vulnerable to various disorders that can impair its normal functioning and affect the quality of life of millions of people around the world. Developing effective treatments for these disorders is a daunting task, as most drugs cannot reach the CNS due to the presence of formidable barriers that protect it from harmful substances. These barriers, namely the blood–brain barrier and the blood–cerebrospinal fluid barrier, are selective and tightly regulated, allowing only certain molecules to cross into the CNS.

This Special Issue aims to shed light on the challenges and opportunities in drug design and delivery for the CNS, showcasing innovative strategies and novel materials that can overcome these barriers and deliver drugs to their desired targets with precision and control. This Special Issue covers a wide range of topics, from understanding the mechanisms and dynamics of the barriers, to designing and synthesizing new drugs and carriers, to evaluating their safety and efficacy in preclinical and clinical studies. The ultimate goal is to unravel the secrets of the CNS and enable transformative therapies that can cure or alleviate the symptoms of neurological and neuropsychiatric disorders. We invite you to join us on this exciting journey to explore the borders of drug delivery for the CNS and discover new ways to improve the health and well-being of patients suffering from these debilitating conditions. We welcome original research and comprehensive review articles that contribute to advancing knowledge and practice in this emerging field.

Dr. Masaru Tanaka
Guest Editor

Manuscript Submission Information

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Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. International Journal of Molecular Sciences is an international peer-reviewed open access semimonthly journal published by MDPI.

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  • central nervous system
  • central nervous system diseases
  • drug delivery systems
  • blood–brain barrier
  • blood–cerebrospinal fluid barrier
  • drug design
  • nanomedicine
  • neuropharmacology
  • neuroprotective agents
  • biomarkers

Published Papers (1 paper)

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16 pages, 5662 KiB  
Systemic Treatment with Fas-Blocking Peptide Attenuates Apoptosis in Brain Ischemia
by Sungeun Chung, Yujong Yi, Irfan Ullah, Kunho Chung, Seongjun Park, Jaeyeoung Lim, Chaeyeon Kim, Seon-Hong Pyun, Minkyung Kim, Dokyoung Kim, Minhyung Lee, Taiyoun Rhim and Sang-Kyung Lee
Int. J. Mol. Sci. 2024, 25(1), 661; https://doi.org/10.3390/ijms25010661 - 4 Jan 2024
Cited by 3 | Viewed by 1450
Apoptosis plays a crucial role in neuronal injury, with substantial evidence implicating Fas-mediated cell death as a key factor in ischemic strokes. To address this, inhibition of Fas-signaling has emerged as a promising strategy in preventing neuronal cell death and alleviating brain ischemia. [...] Read more.
Apoptosis plays a crucial role in neuronal injury, with substantial evidence implicating Fas-mediated cell death as a key factor in ischemic strokes. To address this, inhibition of Fas-signaling has emerged as a promising strategy in preventing neuronal cell death and alleviating brain ischemia. However, the challenge of overcoming the blood–brain barrier (BBB) hampers the effective delivery of therapeutic drugs to the central nervous system (CNS). In this study, we employed a 30 amino acid-long leptin peptide to facilitate BBB penetration. By conjugating the leptin peptide with a Fas-blocking peptide (FBP) using polyethylene glycol (PEG), we achieved specific accumulation in the Fas-expressing infarction region of the brain following systemic administration. Notably, administration in leptin receptor-deficient db/db mice demonstrated that leptin facilitated the delivery of FBP peptide. We found that the systemic administration of leptin-PEG-FBP effectively inhibited Fas-mediated apoptosis in the ischemic region, resulting in a significant reduction of neuronal cell death, decreased infarct volumes, and accelerated recovery. Importantly, neither leptin nor PEG-FBP influenced apoptotic signaling in brain ischemia. Here, we demonstrate that the systemic delivery of leptin-PEG-FBP presents a promising and viable strategy for treating cerebral ischemic stroke. Our approach not only highlights the therapeutic potential but also emphasizes the importance of overcoming BBB challenges to advance treatments for neurological disorders. Full article
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